Onyx Therapeutics, Inc.

Mouhannad Jumaa

Sean Dalziel

Jing Jiang

Christopher J Kirk

Evan Lewis

Katherine A Chu

Naveen Bejugam

Tony Muchamuel

Ying Fang

Peter Shwonek

Zhengping Wang

Jeffrey Joseph Jones

Hansen Wong

Rahul Vishram Manek

Elena T Chan

Sanjeev Sharma

Christopher Justin Kirk

Tony Marcel Muchamuel

This disclosure provides methods for formulating compositions comprising one or more peptide proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin. As well as cyclodextrin complexation methods of formulating a peptide proteasome inhibitor (e.g., a compound of formula (1)-(5) or a pharmaceutically acceptable salt thereof) with one or more cyclodextrins. Such methods substantially increase the solubility and stability of these proteasome inhibitors and facilitate both their manufacture and administration. For example, homogenous solutions of a compound of formula (5) (carfilzomib) can be obtained at a pharmaceutically useful pH (e.g., about 3.5) and at higher concentrations (e.g., about 5 mg/mL) than could be obtained without one or more cyclodextrins and the processes of complexation between the compound and one or more cyclodextrins provided herein. 

Cyclodextrin complexation methods for formulating peptide proteasome inhibitors

This disclosure features modified release pharmaceutical formulations (e.g., extended release pharmaceutical formulations; e.g., solid dosage forms, e.g., tablets) that are useful for the oral administration of oprozomib, or a pharmaceutically acceptable salt thereof, to a human or animal subject as well as methods of making and using the formulations.

Modified release formulations for oprozomib

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Foster City, CA, United States of America

Mouhannad Jumaa